AU2012280246A1 - Heteroaryl-substituted pyrazolopyridines and use thereof as soluble guanylate cyclase stimulators - Google Patents

Heteroaryl-substituted pyrazolopyridines and use thereof as soluble guanylate cyclase stimulators Download PDF

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Publication number
AU2012280246A1
AU2012280246A1 AU2012280246A AU2012280246A AU2012280246A1 AU 2012280246 A1 AU2012280246 A1 AU 2012280246A1 AU 2012280246 A AU2012280246 A AU 2012280246A AU 2012280246 A AU2012280246 A AU 2012280246A AU 2012280246 A1 AU2012280246 A1 AU 2012280246A1
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AU
Australia
Prior art keywords
fluorine
group
alkyl
methyl
trifluoromethyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
AU2012280246A
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English (en)
Inventor
Markus Follmann
Nils Griebenow
Dieter Lang
Gorden Redlich
Johannes-Peter Stasch
Frank Wunder
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Intellectual Property GmbH
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Bayer Intellectual Property GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from DE201110078715 external-priority patent/DE102011078715A1/de
Priority claimed from DE201210200354 external-priority patent/DE102012200354A1/de
Application filed by Bayer Intellectual Property GmbH filed Critical Bayer Intellectual Property GmbH
Publication of AU2012280246A1 publication Critical patent/AU2012280246A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
AU2012280246A 2011-07-06 2012-07-05 Heteroaryl-substituted pyrazolopyridines and use thereof as soluble guanylate cyclase stimulators Abandoned AU2012280246A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE102011078715.1 2011-07-06
DE201110078715 DE102011078715A1 (de) 2011-07-06 2011-07-06 Heteroaryl-substituierte Pyrazolopyridine und ihre Verwendung
DE102012200354.1 2012-01-11
DE201210200354 DE102012200354A1 (de) 2012-01-11 2012-01-11 Heteroaryl-substituierte Pyrazolopyridine und ihre Verwendung
PCT/EP2012/063155 WO2013004785A1 (de) 2011-07-06 2012-07-05 Heteroaryl-substituierte pyrazolopyridine und ihre verwendung als stimulatoren der löslichen guanylatcyclase

Publications (1)

Publication Number Publication Date
AU2012280246A1 true AU2012280246A1 (en) 2014-01-23

Family

ID=46508330

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012280246A Abandoned AU2012280246A1 (en) 2011-07-06 2012-07-05 Heteroaryl-substituted pyrazolopyridines and use thereof as soluble guanylate cyclase stimulators

Country Status (13)

Country Link
US (1) US20140228366A1 (zh)
EP (1) EP2729476B1 (zh)
JP (1) JP6109161B2 (zh)
KR (1) KR20140050029A (zh)
CN (1) CN103906752B (zh)
AU (1) AU2012280246A1 (zh)
BR (1) BR112014000268A2 (zh)
CA (1) CA2840886A1 (zh)
ES (1) ES2648810T3 (zh)
MX (1) MX2014000029A (zh)
RU (1) RU2014103960A (zh)
WO (1) WO2013004785A1 (zh)
ZA (1) ZA201400050B (zh)

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ES2583086T3 (es) 2011-04-21 2016-09-19 Bayer Intellectual Property Gmbh Pirazolopiridinas sustituidas con fluoroalquilo y su uso
SG11201400083VA (en) * 2011-09-02 2014-06-27 Bayer Ip Gmbh Substituted annellated pyrimidine and the use thereof
DE102012200349A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Substituierte annellierte Pyrimidine und Triazine und ihre Verwendung
DE102012200352A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Substituierte, annellierte Imidazole und Pyrazole und ihre Verwendung
DE102012200360A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Substituierte Triazine und ihre Verwendung
CN104395313B (zh) * 2012-03-06 2017-03-08 拜耳知识产权有限责任公司 取代的氮杂双环及其用途
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EP3079700B1 (en) 2013-12-11 2020-11-25 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
MX2016007522A (es) 2013-12-11 2017-12-15 Ironwood Pharmaceuticals Inc Estimuladores de guanilato ciclasa soluble (sgc).
WO2015088885A1 (en) 2013-12-11 2015-06-18 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
EP3094327A1 (en) 2014-01-13 2016-11-23 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
US9796733B2 (en) 2014-06-04 2017-10-24 Merck Sharp & Dohme Corp. Imidazo-pyrazine derivatives useful as soluble guanylate cyclase activators
JP2017529338A (ja) * 2014-08-29 2017-10-05 バイエル・ファルマ・アクティエンゲゼルシャフト アミノ置換環式ピリミジンおよびその使用
WO2016030362A1 (de) 2014-08-29 2016-03-03 Bayer Pharma Aktiengesellschaft Substituierte annellierte pyrimidine und ihre verwendung
TW201625635A (zh) 2014-11-21 2016-07-16 默沙東藥廠 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物
CA2984983A1 (en) 2015-05-06 2016-11-10 Bayer Pharma Aktiengesellschaft The use of sgc stimulators, sgc activators, alone and combinations with pde5 inhibitors for the treatment of digital ulcers (du) concomitant to systemic sclerosis (ssc)
EP3303342B1 (en) 2015-05-27 2021-03-17 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
US10213429B2 (en) 2015-05-28 2019-02-26 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
LT3325013T (lt) 2015-07-23 2020-11-10 Bayer Pharma Aktiengesellschaft Tirpios guanilatciklazės (sgc) stimuliatoriai/aktyvatoriai derinyje su nep inhibitoriumi ir (arba) angiotenzino aii antagonistu ir jų naudojimas
MX2018007152A (es) 2015-12-14 2018-08-15 Ironwood Pharmaceuticals Inc Uso de estimuladores de guanilato ciclasa soluble (sgc) para el tratamiento de la disfuncion del esfinter gastrointestinal.
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
WO2017197555A1 (en) 2016-05-16 2017-11-23 Merck Sharp & Dohme Corp. Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators
WO2017200857A1 (en) 2016-05-18 2017-11-23 Merck Sharp & Dohme Corp. Methods for using triazolo-pyrazinyl soluble guanylate cyclase activators in fibrotic disorders
CN106560180A (zh) * 2016-05-24 2017-04-12 聊城市奥润生物医药科技有限公司 鸟嘌呤核糖苷-3′,5′-环磷酸酯(cGMP)在制备抗肺动脉高压及慢性阻塞性肺病药物中的应用
WO2018069126A1 (de) 2016-10-11 2018-04-19 Bayer Pharma Aktiengesellschaft Kombination enthaltend sgc stimulatoren und mineralocorticoid-rezeptor-antagonisten
EP3525778A1 (de) 2016-10-11 2019-08-21 Bayer Pharma Aktiengesellschaft Kombination enthaltend sgc aktivatoren und mineralocorticoid-rezeptor-antagonisten
EP3554488A2 (en) 2016-12-13 2019-10-23 Cyclerion Therapeutics, Inc. Use of sgc stimulators for the treatment of esophageal motility disorders
CN108727340B (zh) 2017-04-11 2020-12-29 广东东阳光药业有限公司 氟取代的吲唑类化合物及其用途
SG11202011018PA (en) 2018-05-15 2020-12-30 Bayer Ag 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization
JP2021530491A (ja) 2018-07-11 2021-11-11 サイクレリオン・セラピューティクス,インコーポレーテッド ミトコンドリア(mitochonrial)障害の処置のためのsGC刺激剤の使用
WO2020164008A1 (en) 2019-02-13 2020-08-20 Bayer Aktiengesellschaft Process for the preparation of porous microparticles
WO2021219088A1 (zh) * 2020-04-30 2021-11-04 正大天晴药业集团股份有限公司 嘧啶三并环类化合物及其应用
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Also Published As

Publication number Publication date
MX2014000029A (es) 2014-02-17
CN103906752A (zh) 2014-07-02
EP2729476A1 (de) 2014-05-14
RU2014103960A (ru) 2015-08-20
WO2013004785A1 (de) 2013-01-10
CA2840886A1 (en) 2013-01-10
JP2014523895A (ja) 2014-09-18
EP2729476B1 (de) 2017-08-23
JP6109161B2 (ja) 2017-04-05
ES2648810T3 (es) 2018-01-08
KR20140050029A (ko) 2014-04-28
US20140228366A1 (en) 2014-08-14
CN103906752B (zh) 2016-08-24
BR112014000268A2 (pt) 2017-04-25
ZA201400050B (en) 2015-04-29

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Legal Events

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MK5 Application lapsed section 142(2)(e) - patent request and compl. specification not accepted